The -c(=x)- Is Bonded Directly To The Ring Nitrogen Of The Five-membered Hetero Ring (e.g., 1-pyrrolidine Carboxanilides, Etc.) Patents (Class 548/538)
-
Publication number: 20090076125Abstract: The present application describes deuterium-enriched glimepiride, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
-
Publication number: 20080287674Abstract: Compounds useful as intermediates for synthesis of compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification.Type: ApplicationFiled: June 26, 2008Publication date: November 20, 2008Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
-
Publication number: 20080274082Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 24, 2008Publication date: November 6, 2008Inventors: Yonghua Gai, Ying Sun, Yat Sun Or, Zhe Wang
-
Publication number: 20080275021Abstract: The invention relates to pyrrolidine derivatives of formula wherein R1, R2, R3, n, and o are defined in the specification and to pharmaceutically active acid-addition salts thereof. Compounds of formula I have a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.Type: ApplicationFiled: April 14, 2008Publication date: November 6, 2008Inventors: Caterina Bissantz, Torsten Hoffmann, Philippe Jablonski, Henner Knust, Mathias Nettekoven, Hasane Ratni, Xihan Wu
-
Publication number: 20080269221Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: ApplicationFiled: August 10, 2007Publication date: October 30, 2008Inventors: Niels H. Andersen, Jason Bowman, Alice Erwin, Eric Harwood, Toni Kline, Khisimuzi Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
-
Publication number: 20080194633Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: August 1, 2007Publication date: August 14, 2008Inventors: Xiangping Qian, Pu-Ping Lu, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans
-
Patent number: 7407974Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: April 18, 2005Date of Patent: August 5, 2008Assignee: Pfizer Inc.Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
-
Publication number: 20080176838Abstract: The invention relates to compounds of formula (I) wherein R1-9, Z, n, X, A, and Rb have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament for the treatment of type 2 diabetes mellitus, obesity and lipid disorders.Type: ApplicationFiled: June 8, 2005Publication date: July 24, 2008Applicant: SANTHERA PHARMACEUTICALS (DEUTSCHLAND) AGInventors: Paul John Edwards, Silvia Cerezo-Galvez, Achim Feurer, Oliver Hill, Meinolf Thiemann, Victor Giulio Matassa, Sonja Nordhoff, Meritxell Lopez-Canet
-
Publication number: 20080176923Abstract: The invention relates to proline derivatives and their salts, to pharmaceutical agents containing said derivatives and to the use of said agents for treating tumours. The invention also relates to methods for producing said compounds and pharmaceutical agents.Type: ApplicationFiled: December 18, 2003Publication date: July 24, 2008Inventor: Zoser B. Salama
-
Publication number: 20080152619Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: May 9, 2006Publication date: June 26, 2008Inventors: Ny Sin, Paul Michael Scola, Nicholas A. Meanwell, Xiangdong Alan Wang, Li-Qiang Sun, Jie Chen, Andrew Charles Good
-
Patent number: 7365196Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.Type: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
-
Patent number: 7348440Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 12, 2003Date of Patent: March 25, 2008Assignee: Merck & Co., Inc.Inventors: Kenneth L. Arrington, Paul J. Coleman, Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, William F. Hoffman, Edward S. Tasber
-
Patent number: 7304165Abstract: Disclosed are cyclic imino oligomers and polymers comprised of subunits of the formula: Also disclosed are combinatorial libraries and arrays of the cyclic imino compounds.Type: GrantFiled: January 21, 2004Date of Patent: December 4, 2007Assignee: Wisconsin Alumni Research FoundationInventors: Samuel H. Gellman, Bayard R. Huck
-
Patent number: 7291620Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: June 25, 2004Date of Patent: November 6, 2007Assignee: Merck + Co., Inc.Inventors: Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca, Harold G. Selnick
-
Patent number: 7265146Abstract: Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to ?4 integrin receptors and thereby inhibit binding of ligands for ?4 integrins which is useful for prophylactic and/or therapeutic treatment of diseases and conditions associated with ?4 integrins or their ligands.Type: GrantFiled: April 20, 2005Date of Patent: September 4, 2007Assignee: Genentech, Inc.Inventors: Dean R. Artis, David Y. Jackson, Thomas E. Rawson, Mark E. Reynolds, Daniel P. Sutherlin, Mark S. Stanley
-
Patent number: 7262207Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.Type: GrantFiled: February 27, 2004Date of Patent: August 28, 2007Assignee: Abbott LaboratoriesInventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
-
Patent number: 7235580Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: October 14, 2003Date of Patent: June 26, 2007Assignee: Merck & Co., Inc.Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, George D. Hartman, Brenda J. Mariano
-
Patent number: 7211666Abstract: Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described in the specification. The methods according to the invention utilize an amination process, in which a pyrrole is reacted with a haloamine, preferably chloramine. This step is followed by cyclization to form the pyrrolotriazine core.Type: GrantFiled: December 22, 2004Date of Patent: May 1, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Jollie Duaine Godfrey, Jr., John Hynes, Jr., Alaric J. Dyckman, Katerina Leftheris, Zhongping Shi, Stephen T. Wrobleski, Wendel William Doubleday, John A. Grosso
-
Patent number: 7160877Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower-alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.Type: GrantFiled: June 22, 2004Date of Patent: January 9, 2007Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
-
Patent number: 7157585Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: May 11, 2005Date of Patent: January 2, 2007Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
-
Patent number: 7094909Abstract: The present invention concerns processes for preparing compounds of formula (I-H), or a prodrug, pharmaceutically active metabolite, or pharmaceutically active salt or solvate thereof, which are useful as inhibitors of the HIV protease enzyme.Type: GrantFiled: December 4, 2003Date of Patent: August 22, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: David John Kucera, Robert William Scott
-
Patent number: 7084139Abstract: The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.Type: GrantFiled: June 6, 2002Date of Patent: August 1, 2006Assignee: SmithKline Beecham CorporationInventors: Chuen Chan, Julie Nicole Hamblin, Henry Anderson Kelly, Nigel Paul King, Andrew McMurtrie Mason, Vipulkumar Kantibhai Patel, Stefan Senger, Gita Punjabhai Shah, Nigel Stephen Watson, Helen Elisabeth Weston, Caroline Whitworth, Robert John Young
-
Patent number: 7030141Abstract: The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: October 23, 2002Date of Patent: April 18, 2006Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
-
Patent number: 6992102Abstract: The invention provides compounds of the formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds.Type: GrantFiled: October 14, 2003Date of Patent: January 31, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Lawrence Hamann, David Augeri, Chongqing Sun, Jeffrey A. Robl, Mark E. Salvati, Tammy Wang
-
Patent number: 6906046Abstract: Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-? and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.Type: GrantFiled: December 11, 2001Date of Patent: June 14, 2005Assignee: Celltech R & D Inc.Inventors: Randy W. Jackson, Ihab Darwish, Ted A. Baughman, J. Jeffry Howbert
-
Patent number: 6903116Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequenc in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.Type: GrantFiled: January 9, 2003Date of Patent: June 7, 2005Assignee: Kaneka Corp.Inventors: Shin-ichi Yokota, Kozo Yamamoto, Souichi Morikawa, Yoshihide Fuse, Mikio Kitahara
-
Patent number: 6900238Abstract: Combinatorial libraries of HIV and FIV protease inhibitors are characterized by ?-keto amide or hydroxyethylamine core structures flanked by on one side by substituted pyrrolidines, piperidines, or azasugars and on the other side by phenylalanine, tyrosine, or substituted tyrosines. The libraries are synthesized via a one step coupling reaction. Highly efficacious drug candidates are identified by screening the libraries for binding and inhibitory activity against both HIV and FIV protease. Drug candidates displaying clinically useful activity against both HIV and FIV protease are identified as being potentially resistive against a loss of inhibitory activity due to development of resistant strains of HIV.Type: GrantFiled: December 9, 1996Date of Patent: May 31, 2005Assignee: The Scripps Research InstituteInventors: Chi-Huey Wong, Deborah H. Slee, Karen Laslo
-
Patent number: 6852752Abstract: Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptide deformylase (PDF), an enzyme present in prokaryotes and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.Type: GrantFiled: December 13, 2000Date of Patent: February 8, 2005Assignee: Vicuron Pharmaceuticals Inc.Inventors: Jeffrey W. Jacobs, Dinesh Patel, Jason Lewis, Zhi-Jie Ni
-
Patent number: 6838565Abstract: Carboxylic acid amides of general formula having an antithrombotic activity and a factor Xa-inhibiting activity. Exemplary are: (a) N-[1-(3-amidino-phenyl)-2-(1H-tetrazol-5-yl)-ethyl]-4-(2,5-dihydro-pyrrol-1-yl-carbonyl)-3-methyl-benzamide, (b) N-[1-(3-amidino-phenyl)-2-(1H-tetrazol-5-yl)-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide, (c) N-[1-(5-amidino-2-hydroxy-phenyl)-2-phenyl-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide, and (d) N-[1-(5-amidino-2-hydroxy-phenyl)-2-(pyridin-3-yl)-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide.Type: GrantFiled: July 21, 2003Date of Patent: January 4, 2005Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Uwe Ries, Henning Priepke, Wolfgang Wienen, Herbert Nar, Sandra Handschuh
-
Patent number: 6762178Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.Type: GrantFiled: June 14, 2001Date of Patent: July 13, 2004Assignee: Wyeth Holdings CorporationInventors: Jeremy I. Levin, James M. Chen
-
Patent number: 6727368Abstract: Disclosed are cyclic imino oligomers and polymers comprised of subunits of the formula: Also disclosed are combinatorial libraries and arrays of the cyclic imino compounds.Type: GrantFiled: June 13, 2000Date of Patent: April 27, 2004Assignee: Wisconsin Alumni Research FoundationInventors: Samuel H. Gellman, Bayard R. Huck, Michele R. Richards
-
Publication number: 20040072892Abstract: A cyanopyrrolidine derivative represented by Formula (1): 1Type: ApplicationFiled: November 3, 2003Publication date: April 15, 2004Inventors: Hiroshi Fukushima, Akira Hiratate, Masato Takahashi, Kazuya Kameo
-
Patent number: 6710186Abstract: Disclosed are cyclic imino oligomers and polymers comprised of subunits of the formula: Also disclosed are combinatorial libraries and arrays of the cyclic imino compounds.Type: GrantFiled: June 18, 2001Date of Patent: March 23, 2004Assignee: Wisconsin Alumni Research FoundationInventors: Samuel H. Gellman, Bayard R. Huck
-
Patent number: 6706753Abstract: Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to &agr;4 integrin receptors and thereby inhibit binding of ligands for &agr;4 integrins which is useful for prophylactic and/or therapeutic treatment of diseases and conditions associated with &agr;4 integrins or their ligands.Type: GrantFiled: December 6, 2002Date of Patent: March 16, 2004Assignee: Genentech, Inc.Inventors: Dean R. Artis, David Y. Jackson, Thomas E. Rawson, Mark E. Reynolds, Daniel P. Sutherlin, Mark S. Stanley
-
Publication number: 20040002609Abstract: The present invention relates to a method of making novel dipeptidyl peptidase-IV (“DPP-IV’) inhibitor compounds useful for treating, inter alia, diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, metabolic syndrome (Syndrome X or insulin resistance syndrome), hyperglycemia, impaired glucose tolerance, glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of making 3,3,4,4-tetrafluoropyrrolidine, a starting material utilized in the afore-mentioned method for preparing DPP-IV compounds.Type: ApplicationFiled: June 3, 2003Publication date: January 1, 2004Applicant: Pfizer Inc.Inventor: Bernard Hulin
-
Patent number: 6664400Abstract: The present invention relates to a compound of Formula 3 wherein X is H, F or Cl; Y is F or Cl; R1 is C1-C3 haloalkyl, C2-C4 alkoxyalkyl; C2-C6 haloalkoxyalkyl or C2-C6 cyanoalkyl; R2 is H, C1-C4 alkyl, C1-C4 haloalkyl, C3-C4 alkenyl, C3-C4 alkynyl, C2-C4 alkoxyalkyl, C2-C4 alkylcarbonyl or C2-C4 alkoxycarbonyl; R3 is H or OH; and R4 is H, F or Cl; provided that when R3 is H then R4 is F or Cl and when R3 is OH then R4 is H.Type: GrantFiled: January 4, 2002Date of Patent: December 16, 2003Assignee: Degussa AGInventors: Eric Deguyon Taylor, Viacheslav Alexandrovich Petrov, Matthias Schaeffer, Karlheinz Drauz, Anne Vogt, Christoph Weckbecker, Steven H. Swearingen, Balreddy Kamireddy
-
Publication number: 20030166681Abstract: The present invention is directed to compounds useful as selective serine protease or dual-serine protease inhibitors, compositions thereof and methods for treating serine protease or dual-serine protease mediated disorders.Type: ApplicationFiled: November 25, 2002Publication date: September 4, 2003Inventors: Michael N. Greco, Bruce E. Maryanoff, Michael J. Hawkins, Robert E. Boyd
-
Publication number: 20030166680Abstract: The present invention is directed to compounds useful as selective serine protease or dual-serine protease inhibitors, compositions thereof and methods for treating serine protease or dual-serine protease mediated disorders.Type: ApplicationFiled: November 25, 2002Publication date: September 4, 2003Inventors: Michael N. Greco, Bruce E. Maryanoff, Michael J. Hawkins, Robert E. Boyd
-
Patent number: 6613780Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequence in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.Type: GrantFiled: August 27, 2001Date of Patent: September 2, 2003Assignee: Kaneka CorporationInventors: Shin-ichi Yokota, Kozo Yamamoto, Souichi Morikawa, Yoshihide Fuse, Mikio Kitahara
-
Patent number: 6607868Abstract: Dipropargyl acetamide derivatives of following Formula 1 which are photoresist monomers, polymers thereof, and photoresist compositions containing the same. The photoresist polymer has high etching resistance, adhesiveness and post-exposure delay stability. As a result, the photoresist composition is suitable to form a fine pattern in a deep ultraviolet region. wherein, n is an integer from 0 to 5.Type: GrantFiled: June 25, 2001Date of Patent: August 19, 2003Assignee: Hynix Semiconductor Inc.Inventor: Jae Hak Choi
-
Publication number: 20030096857Abstract: Compounds which are 1-(2′-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2,3 and 4); X is selected from aminoacyl groups corresponding to the natural amino acids, acyl groups R3CO, groups R4COOC(R5)(R6)OCO, methoxycarbonyl, ethoxycarbonyl and benzyloxycarbonyl; R1 is selected from H, C1-C6 alkyl residues, (CH2)aNHW1, (CH2)bCOW2, (CH2)cOW3, CH(Me)OW4, (CH2)d—C6H4—W5 and (CH2)eSW6, where a is 2-5, b is 1-4, c is 1-2, d is 1-2, e is 1-3, W1 is COW6, CO2W6 or SO2W6, W2 is OH, NH2, OW6 or NHW6, W3 is H or W6, W4 is H or W6, W5 is H, OH or OMe, and W6 is C1-C6 alkyl, optionally substituted phenyl, optionally substituted heteroaryl or benzyl and R2 is selected from H and (CH2)n—C5H3N—Y, where n is 2-4 and Y is H, F, Cl, NO2 or CN, or R1 and R2 together are —(CH2)p-where p is 3 or 4; R3 is selected from H, C1-C6 alkyl and phenyl; R4 isType: ApplicationFiled: June 20, 2002Publication date: May 22, 2003Inventor: David Michael Evans
-
Patent number: 6534536Abstract: Alkylsulfonamido heterocyclic thrombin inhibitors are provided which have the structure wherein G is wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; R is hydrogen, hydroxyalkyl, aminoalkyl, alkyl, cycloalkyl, amidoalkyl, arylalkyl, alkenyl, aryl, alkynyl, arylalkoxyalkyl, or an amino acid side chain; R1 and R2 are independently hydrogen, lower alkyl, cycloalkyl, aryl, hydroxy, alkoxy, oxo, thioketal, thioalkyl, thioaryl, amino or alkylamino; or R1 and R2 can be taken together with the carbons to which they are attached to form a cycloalkyl, aryl or heteroaryl ring.Type: GrantFiled: March 16, 1994Date of Patent: March 18, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Spencer D. Kimball, Jagabandhu Das, Wan Fang Lau
-
Patent number: 6531612Abstract: Compounds of the formula: wherein R1 to R7 and Y are as defined in the specification, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof, are useful for treating diseases associated with cystein proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.Type: GrantFiled: December 21, 2000Date of Patent: March 11, 2003Assignee: Hoffman-La Roche Inc.Inventors: Tobias Gabriel, Michael Pech, Sabine Wallbaum
-
Patent number: 6515011Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. where R3 is —CH2NH2, —CH2CH2NH2, or —CH2NHC(O)OC(CH3)3.Type: GrantFiled: December 18, 2001Date of Patent: February 4, 2003Assignee: Merck & Co., Inc.Inventors: Harold G. Selnick, James C. Barrow, Philippe G. Nantermet, Peter D. Williams, Kenneth J. Stauffer, Philip E. Sanderson, Kenneth E. Rittle, Matthew M. Morrissette, Catherine M. Wiscount, Lekhanh O. Tran, Terry A. Lyle, Donnette D. Staas
-
Patent number: 6512120Abstract: This invention is directed to methods of synthesizing densely functionalized pyrrolidine compounds through the use of intramolecular Diels Alder reactions.Type: GrantFiled: March 12, 2002Date of Patent: January 28, 2003Assignee: Ortho McNeil Pharmaceutical, Inc.Inventors: Pranab Mishra, Sengen Sun, William V. Murray
-
Patent number: 6423689Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.Type: GrantFiled: December 16, 1998Date of Patent: July 23, 2002Assignees: Warner-Lambert Company, Neurex CorporationInventors: Richard John Booth, Louis Brogley, Wayne Livingston Cody, David Thomas Connor, Harriet Wall Hamilton, John Xiaoqiang He, Lain-Yen Hu, Leonard Joseph Lescosky, Thomas Charles Malone, Laszlo Nadasdi, Michael Francis Rafferty, Bruce David Roth, Diego F. Silva, Yuntao Song, Balazs G. Szoke, Laszlo Urge
-
Patent number: 6403612Abstract: A thrombin receptor antagonist having the formula or a pharmaceutically acceptable salt thereof, useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non-toxic amount of such compound to a mammal, preferably a human.Type: GrantFiled: January 30, 2001Date of Patent: June 11, 2002Assignee: Merck & Co., Inc.Inventors: Philippe G. Nantermet, James C. Barrow, Harold G. Selnick
-
Patent number: 6362204Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; and R5 is a group —L2(CH2)tR6 in which L2 is a —N(R7)CO— or —N(R7)CS— group. The compounds are able to inhibit the binding &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: May 20, 1999Date of Patent: March 26, 2002Assignee: Celltech Therapeutics, LtdInventors: John Clifford Head, Sarah Catherine Archibald, Graham John Warrellow, John Robert Porter
-
Publication number: 20020012879Abstract: Dipropargyl acetamide derivatives of following Formula 1 which are photoresist monomers, polymers thereof, and photoresist compositions containing the same. The photoresist polymer has high etching resistance, adhesiveness and post-exposure delay stability. As a result, the photoresist composition is suitable to form a fine pattern in a deep ultraviolet region.Type: ApplicationFiled: June 25, 2001Publication date: January 31, 2002Inventor: Jae Hak Choi
-
Patent number: RE40183Abstract: The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula wherein R, X, R5 and R6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.Type: GrantFiled: June 3, 2005Date of Patent: March 25, 2008Assignee: Wyeth Holdings CorporationInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross